Assay Detail
Binding
CHEMBL828795
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Inhibitory activity against human carbonic anhydrase II expressed in Escherichia coli BL21
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating 1,2,4-triazine moieties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 7.45 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL220491 | BRINZOLAMIDE | 4.0 | 1 | 8.52 |
| CHEMBL18 | ETHOXZOLAMIDE | 4.0 | 1 | 8.10 |
| CHEMBL218490 | DORZOLAMIDE | 4.0 | 1 | 8.05 |
| CHEMBL20 | ACETAZOLAMIDE | 4.0 | 1 | 7.92 |
| CHEMBL187901 | — | — | 1 | 7.89 |
| CHEMBL19 | METHAZOLAMIDE | 4.0 | 1 | 7.85 |
| CHEMBL77517 | INDISULAM | 2.0 | 1 | 7.82 |
| CHEMBL186504 | — | — | 1 | 7.82 |
| CHEMBL363543 | — | — | 1 | 7.70 |
| CHEMBL187274 | — | — | 1 | 7.68 |
| CHEMBL184923 | — | — | 1 | 7.68 |
| CHEMBL366086 | — | — | 1 | 7.64 |
| CHEMBL186716 | — | — | 1 | 7.64 |
| CHEMBL184107 | — | — | 1 | 7.57 |
| CHEMBL365860 | — | — | 1 | 7.44 |
| CHEMBL17 | DICHLORPHENAMIDE | 4.0 | 1 | 7.42 |
| CHEMBL183945 | — | — | 1 | 7.08 |
| CHEMBL359997 | — | — | 1 | 7.01 |
| CHEMBL366069 | — | — | 1 | 6.97 |
| CHEMBL185549 | — | — | 1 | 6.95 |
| CHEMBL185473 | — | — | 1 | 6.89 |
| CHEMBL7087 | — | — | 1 | 6.80 |
| CHEMBL419 | MAFENIDE | 4.0 | 1 | 6.77 |
| CHEMBL183153 | — | — | 1 | 6.56 |
| CHEMBL21 | SULFANILAMIDE | 4.0 | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL220491 | BRINZOLAMIDE | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL18 | ETHOXZOLAMIDE | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL218490 | DORZOLAMIDE | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL20 | ACETAZOLAMIDE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL187901 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL19 | METHAZOLAMIDE | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL77517 | INDISULAM | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL186504 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL363543 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL187274 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL184923 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL366086 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL186716 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL184107 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL365860 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL17 | DICHLORPHENAMIDE | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL183945 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL359997 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL366069 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL185549 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL185473 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL7087 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL419 | MAFENIDE | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL183153 | — | Ki | = | 278.0 | nM | 6.56 |
| CHEMBL21 | SULFANILAMIDE | Ki | = | 300.0 | nM | 6.52 |